Search Result
Results for "
relaxation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
7
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-161152
-
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DNA/RNA Synthesis
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Cancer
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DNA relaxation-IN-1 (compound 27) is a DNA Ligase 1 (DNA Lig1) inhibitor, which inhibits DNA ligation and disrupts Lig I’s DNA relaxation activity. DNA relaxation-IN-1 combined with Topotecan (HY-13768) exhibits a synergistic antiproliferative effect on colorectal cancer cells .
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- HY-P0102
-
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mAChR
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Neurological Disease
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Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation .
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-
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- HY-137466
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Topoisomerase
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Cancer
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ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
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-
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- HY-148516
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Myosin
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Neurological Disease
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MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. MPH-220 enables muscle relaxation. MPH-220 is anti-spastic agent that can be used in the research of spasticity and muscle stiffness .
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-
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- HY-B0740
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MK130 hydrochloride
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5-HT Receptor
Parasite
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Infection
Neurological Disease
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Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
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-
-
- HY-148516A
-
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Myosin
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Neurological Disease
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(R)-MPH-220 is the R isomer of MPH-220 (HY-148516). MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. MPH-220 enables muscle relaxation. MPH-220 is anti-spastic agent that can be used in the research of spasticity and muscle stiffness .
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- HY-N2646
-
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Fungal
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Infection
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5-Heptadec-cis-8-enylresorcinol is a 5-alkylresorcinol that can be isolated from etiolated rice seedlings. 5-Heptadec-cis-8-enylresorcinol is an antifungal agent against the rice blast fungus. 5-Heptadec-cis-8-enylresorcinol mediates DNA relaxation .
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-
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- HY-106684A
-
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Adrenergic Receptor
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Cardiovascular Disease
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Ridazolol hydrochloride is a β-adrenergic receptor (βAR) antagonist. Ridazolol hydrochloride exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol hydrochloride can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol hydrochloride is utilized in the research of cardiovascular diseases .
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- HY-106684
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Adrenergic Receptor
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Cardiovascular Disease
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Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases .
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- HY-124950
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GR114297A
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Adrenergic Receptor
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Others
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Picumeterol (GR114297A) is a potent and selective β2-adrenoceptor agonist with bronchodilator and anti-bronchoconstrictor effects. Picumeterol produces long-lasting relaxation of airways smooth muscle both in vitro and in vivo. Picumeterol is cleared from plasma through a rapid and extensive hepatic metabolism. Picumeterol is proming for rasearch of asthma and related diseases .
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- HY-129445
-
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Potassium Channel
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Cardiovascular Disease
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SG-209 is a Nicorandil (HY-B0341) derivative that produces relaxation through potassium channel activation, while this action contributes to the vasodilating action of Nicorandil (HY-B0341) at higher concentrations. SG-209 dilates tracheal smooth muscle and increases tracheal blood flow in anesthetized dogs .
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- HY-108760
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Gd-DOTA; Magnescope; P-449
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Biochemical Assay Reagents
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Cardiovascular Disease
Others
Neurological Disease
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Gadoterate meglumine (Gd-DOTA) is a non-specific paramagnetic gadolinium complex used as a contrast enhancer in magnetic resonance imaging (MRI). Gadoterate meglumine, as a contrast agent in MRI, is able to shorten the longitudinal relaxation time (T1) of tissue, resulting in a brighter signal in MRI images. Gadoterate meglumine can be used for the study of the central nervous system (such as the brain and spinal cord), abdominal, pelvic organs, breast, bone and joint imaging, angiography, and cardiac electrophysiology .
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- HY-117657
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Topoisomerase
Bacterial
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Inflammation/Immunology
Cancer
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(-)-BO 2367, an antimicrobial quinolone, is a strong mammalian and bacterial topoisomerase II inhibitor. (-)-BO 2367 shows IC50 values with 3.8 μM, 0.5 μM, and 1 μM against the DNA relaxation activity of L1210 topoisomerase II and the supercoiling activities of Escherichia coli gyrase and Micrococcus luteus gyrase, respectively. (-)-BO 2367 is a potent antitumor agent .
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- HY-121146
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-
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- HY-P4766
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CGRP Receptor
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Cardiovascular Disease
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Adrenomedullin (porcine) is a peptide that regulates vasodilation. Adrenomedullin (porcine) induces endothelium-dependent relaxation in rat aorta with IC50 value of 2.4 nM. Adrenomedullin (porcine) induces endothelium-independent relaxation of porcine coronary arteries with an IC50 of 27.6 nM .
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- HY-134004
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Carbetapentane
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
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- HY-B1055
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Carbetapentane citrate
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
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- HY-134004R
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
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- HY-B1700B
-
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Others
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Neurological Disease
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(S,S)-Mivacurium dichloride (Compound 29a) is a neuromuscular blocking agent and causes muscle relaxation .
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- HY-B1055R
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Sigma Receptor
mAChR
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Neurological Disease
Inflammation/Immunology
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Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].
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- HY-G0008
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Mebeverine metabolite O-desmethyl Mebeverine alcohol
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Adrenergic Receptor
Drug Metabolite
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Metabolic Disease
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O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
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- HY-130673
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NO Synthase
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Cardiovascular Disease
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L-NABE is a nitric oxide (NO) synthase inhibitor. L-NABE is also a potent endothelium dependent vasoconstrictor and inhibitor of relaxation .
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- HY-G0008A
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Mebeverine metabolite O-desmethyl Mebeverine alcohol hydrochloride
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Adrenergic Receptor
Drug Metabolite
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Metabolic Disease
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O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
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- HY-19583
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- HY-103148
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5-HT Receptor
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Neurological Disease
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LY215840, a 5-HT7 receptor ligand and a 5-HT2 receptor antagonist, blocks serotonin-induced relaxation in canine coronary artery .
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- HY-106908
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WAY-PDA 641
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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WAY-PDA 641 is a potent and preferential PDE-IV inhibitor, with an IC50 of 0.42 μM for canine trachealis PDE-IV. WAY-PDA 641 induces respiratory muscle relaxation and bronchodilation .
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- HY-101952
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-
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- HY-19548
-
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Arginase
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Endocrinology
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BEC, an arginine analogue, is a slow-binding competitive inhibitor of the binuclear manganese metalloenzyme arginase. BEC enhances substrate flux to NO synthase, thereby enhancing NO-dependent smooth muscle relaxation in the corpus cavernosum, and enhances penile erection .
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- HY-N8444
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Interleukin Related
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Cardiovascular Disease
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Triptoquinone A, an interleukin 1 inhibitor, inhibits endomycin (LPS) or interleukin (IL-1β)-promoted induction of nitric oxide synthase (NOS) in vascular smooth muscle, thereby inhibiting Arg-induced vascular relaxation .
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- HY-N3488
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Topoisomerase
Bacterial
Fungal
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Infection
Cancer
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Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities .
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- HY-14464
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-
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- HY-101826A
-
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Phosphodiesterase (PDE)
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Cancer
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ER21355 hydrochloride is the hydrochloride form of ER21355 (HY-101826). ER21355 hydrochloride is an inhibitor for phosphodiesterase (PDE), which is potent for ameliorating benign prostatic hyperplasia (BPH) and prostatism through increasing levels of cAMP and cGMP, and resulting a relaxation of the smooth muscle cell .
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- HY-124363
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-
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- HY-162511
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Dopamine Transporter
Serotonin Transporter
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Others
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IP2015 is an inhibitor for monoamine reuptake, that inhibits the reuptake of dopamine, serotonin (5-HT), and noradrenaline. IP2015 increases release of central dopamine and peripheral nitric oxide (NO), causes the NO-mediated relaxation of erectile tissue, and thus induces erection in rat model .
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- HY-162733
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Microtubule/Tubulin
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Cardiovascular Disease
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SVC-02 is a vasohibin (VASH) inhibitor with an IC50 value of 11 nM. SVC-02 reduces tubulin detyrosination. SVC-02 has the potential for the research of reduce myo-cardial stiffness and improve relaxation in Heart failure with preserved ejection fraction (HFpEF) .
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- HY-N0484
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Autophagy
Mitophagy
Apoptosis
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Cardiovascular Disease
Cancer
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Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc .
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- HY-142972
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Prostaglandin Receptor
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Cardiovascular Disease
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19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels .
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- HY-W012980
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Endogenous Metabolite
AMPK
PKA
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Metabolic Disease
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Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
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- HY-P10549
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Endogenous Metabolite
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Neurological Disease
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NGFFFamide is a muscle-active neuropeptide found in sea urchins. NGFFFamide regulates muscle activity by directly interacting with receptor proteins on muscle cells, or indirectly by stimulating nerves or other cell types to release muscle-active factors. NGFFFamide can be used to study muscle contraction and relaxation .
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- HY-169871
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iGluR
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Neurological Disease
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Argiotoxin 636 is a toxin and the non-specific, non-competitive, and potent ionotropic glutamate receptor (iGluR) antagonist. Argiotoxin 636 blocks excitatory synaptic transmission in neurons and has paralysis and muscle relaxation effects. Argiotoxin 636 can be used in the study of nervous system diseases .
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- HY-18351A
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LMP-400 hydrochloride; NSC-724998 hydrochloride
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Topoisomerase
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Infection
Cancer
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Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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- HY-B1283
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iGluR
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Neurological Disease
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Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm .
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- HY-128043
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AY-23578; Doproston B; 11-Deoxy-PGE1
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Prostaglandin Receptor
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Inflammation/Immunology
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11-Deoxy prostaglandin E1 (AY-23578; Doproston B) is an analog of prostaglandin E1 (PGE1) with bronchodilator activity. 11-Deoxy prostaglandin E1 inhibits histamine-induced bronchoconstriction and causes relaxation of tracheal strips in isolated guinea pigs .
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- HY-120954
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Endogenous Metabolite
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Cardiovascular Disease
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14,15-EE-5(Z)-E is a structural analogue of 14, 15-epoxide dicartrienoic acid (14,15-EET). 14,15-EE-5(Z)-E antagonizes the relaxation of vascular smooth muscle induced by EET .
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- HY-N10881
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Others
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Cardiovascular Disease
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Dihydrocurcumenone is a carabrane-type sesquiterpene. Dihydrocurcumenone can be isolated from Curcuma zedoaria, and the common form is 4-dihydrocurcumenone. Curcuma zedoaria sesquiterpene has vascular relaxation activity. 4-dihydrocurcumenone can inhibit the high concentration of K + induced constriction of isolated rat aortic strips .
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- HY-18351
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LMP-400; NSC-724998
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Topoisomerase
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Infection
Cancer
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Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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- HY-N10495
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Antibiotic
Bacterial
Topoisomerase
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Infection
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Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics .
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- HY-B1209
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7-(β-Hydroxyethyl)theophylline
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Phosphodiesterase (PDE)
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Cardiovascular Disease
Inflammation/Immunology
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Etofylline (7-(β-Hydroxyethyl) theophylline) is an oral bronchodilator with anti-inflammatory effects. Etofylline inhibits phosphodiesterase and prevents the degradation of cAMP (cyclic adenosine monophosphate), leading to smooth muscle relaxation, reducing inflammatory responses and improving respiratory function. Etofylline affects the development of zebrafish embryos .
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- HY-N1620
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-
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- HY-B1481A
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Isoetarine
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Adrenergic Receptor
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Cardiovascular Disease
Inflammation/Immunology
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Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
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- HY-B1481
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Isoetarine mesylate
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Adrenergic Receptor
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Cardiovascular Disease
Inflammation/Immunology
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Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator .
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- HY-101952R
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PGE2(Standard); Dinoprostone (Standard)
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Prostaglandin Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Prostaglandin E2 (Standard) is the analytical standard of Prostaglandin E2. This product is intended for research and analytical applications. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
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- HY-171187
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CL 13580
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Carbonic Anhydrase
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Cancer
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Chlorzolamide (CL 13580) is a carbonic anhydrase (CA) inhibitor. Chlorzolamide has an effect on the skeletal muscle of rats, which can reduce the tetanic contraction force of soleus and extensor digitorum longus and prolong the relaxation time and peak time of muscle contraction. In addition, Chlorzolamide inhibits tumor cell proliferation and has antitumor activity .
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- HY-14780
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NXL 101
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Antibiotic
Topoisomerase
DNA/RNA Synthesis
Bacterial
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Infection
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Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L .
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- HY-101952S1
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-
- HY-107416
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U-57908
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DAGL
Acyltransferase
mAChR
COX
Phospholipase
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Neurological Disease
Metabolic Disease
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RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC) .
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- HY-101952S
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PGE2-d4; Dinoprostone-d4
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Prostaglandin Receptor
Endogenous Metabolite
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Cardiovascular Disease
Endocrinology
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Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
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- HY-19641
-
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Biochemical Assay Reagents
Prostaglandin Receptor
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Others
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AH13205 is a selective prostanoid EP2-receptor agonist. AH13205 causes concentration-related relaxations of Carbachol (HY-B1208)-contracted trachea. AH13205 causes dose-related protection against Histamine (HY-B1204)-induced increases in respiratory rate .
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- HY-167091
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(Rac)-TRK-100 free acid; (Rac)-ML 1229
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Prostaglandin Receptor
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Cardiovascular Disease
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(Rac)-Beraprost ((Rac)-ML 1229) is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
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- HY-129210
-
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Phosphodiesterase (PDE)
Potassium Channel
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Cardiovascular Disease
|
KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K + channels. KMUP-4 can be used in the study of cardiovascular diseases .
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- HY-B1283S
-
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Isotope-Labeled Compounds
iGluR
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Neurological Disease
|
Mephenesin-d3 is deuterium labeled Mephenesin. Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm .
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- HY-147384
-
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Calcium Channel
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Cardiovascular Disease
|
CXL-1020 is a hydroxylamine-based nitroxyl (HNO) donor. CXL-1020 improves cardiac inotropy/lusitropy and Ca 2+ cycling in rats with abnormal relaxation. CXL-1020 induces vasorelaxation and improves cardiac function in canine models. CXL-1020 has been used to research systolic heart failure and stable heart failure .
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- HY-W012980R
-
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Endogenous Metabolite
AMPK
PKA
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Metabolic Disease
|
Isovaleric acid (Standard) is the analytical standard of Isovaleric acid. This product is intended for research and analytical applications. Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
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- HY-W127670
-
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Biochemical Assay Reagents
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Others
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Decamethonium (iodide) is an organic compound containing ammonium and iodide ions. It is commonly used as a neuromuscular blocking agent in anesthesia to induce muscle relaxation during surgery. Decamethonium Iodide acts by binding to nicotinic acetylcholine receptors (nAChRs) in the neuromuscular junction, causing depolarization block and subsequent skeletal muscle paralysis. In addition, it can also serve as a reference standard for pharmacological studies of nAChRs.
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- HY-B0394
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Tropine tropate sulfate monohydrate; DL-Hyoscyamine sulfate monohydrate
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mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
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- HY-167203
-
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Calcium Channel
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Cardiovascular Disease
|
AJG049 free base is a calcium channel (Ca 2+ channel) antagonist. AJG049 free base regulates vascular relaxation, reduces cardiac load, and improves cardiac perfusion by binding to the binding site of L-type calcium channels, specifically Diltiazem (HY-B0632). AJG049 free base can be used in cardiovascular disease research .
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- HY-B1205B
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Tropine tropate hydrobromide; DL-Hyoscyamine hydrobromide
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mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) hydrobromide is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine hydrobromide inhibits ACh-induced relaxations in human pulmonary veins. Atropine hydrobromide can be used for research of anti-myopia and bradycardia .
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-
- HY-B1205A
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Tropine tropate sulfate; DL-Hyoscyamine sulfate; Sulfatropinol
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mAChR
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
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-
- HY-P1016
-
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Endothelin Receptor
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Cardiovascular Disease
|
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 1 2.
|
-
- HY-N0485
-
|
Autophagy
Mitophagy
|
Cardiovascular Disease
|
Liensinine Diperchlorate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlorate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlorate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc .
|
-
- HY-N11538
-
|
Others
|
Inflammation/Immunology
|
Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside is a orally active phenolic compound that can be isolated from the Geranium species. Quercetin-3-O-(2′′-O-galloyl)-β-D-glucopyranoside has anti-inflammatory activities and has potential application in edema and aortic endothelium-dependent relaxation injury .
|
-
- HY-124950A
-
(+)-GR114297A
|
Adrenergic Receptor
|
Metabolic Disease
|
(+)-Picumeterol is a configurations of Picumeterol (HY-124950). Picumeterol is a potent and selective β2-adrenoceptor agonist with bronchodilator and anti-bronchoconstrictor effects .
|
-
- HY-118689
-
|
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation .
|
-
- HY-103316
-
|
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis .
|
-
- HY-10061
-
AZD-3355
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-10061B
-
AZD-3355 hydrochloride
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-P1016B
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
|
-
- HY-122215
-
N-696
|
Adrenergic Receptor
|
Endocrinology
|
Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats .
|
-
- HY-108047
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
|
MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor. MK-0873 increases intracellular levels of cyclic adenosine phosphate (cAMP) by inhibiting the activity of the PDE4 enzyme and subsequently activates protein kinase A (PKA). Activated PKA inhibits the activity of inflammatory cells and leads to direct relaxation of airway smooth muscle. MK-0873 can be used in studies of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-10061A
-
AZD-3355 napadisylate
|
GABA Receptor
|
Metabolic Disease
|
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
|
-
- HY-Z7721
-
(Rac)-TRK-100; (Rac)-ML 1129 sodium
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
(Rac)-Beraprost ((Rac)-ML 1129) sodium is a racemic isomer of Beraprost sodium (HY-13569A). Beraprost sodium is an orally active prostacyclin analog that inhibits the release of Ca 2+ from intracellular storage sites by binding to prostacyclin membrane receptors (Prostaglandin Receptor), leading to relaxation of smooth muscle cells and vasodilation. Beraprost sodium has vasodilatory, antiplatelet, and cytoprotective effects, making it promising for research in the field of cardiovascular diseases, such as thromboangiitis obliterans and atherosclerosis .
|
-
- HY-101222
-
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
|
-
- HY-B1640A
-
Etacrynic acid sodium; Sodium etacrynate
|
NF-κB
Glutathione S-transferase
Calcium Channel
NO Synthase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Ethacrynic acid (Etacrynic acid sodium) sodium is a diuretic. Ethacrynic acid sodium is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid sodium is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid sodium also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid sodium has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-125626
-
8-iso-15-keto PGF2α
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a partial agonist for Thromboxane receptor (TP), which exhibits a vasoconstrictor efficacy with a pD2 of 5.8. 8-iso-15-keto Prostaglandin F2α mediates a weak relaxation of rats aorta rings at high concentration .
|
-
- HY-110137A
-
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
|
-
- HY-110137
-
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
|
-
- HY-108538
-
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-B0740R
-
MK130 hydrochloride (Standard)
|
5-HT Receptor
|
Neurological Disease
|
Cyclobenzaprine (MK130) hydrochloride (Standard) is the analytical standard of Cyclobenzaprine (MK130) hydrochloride. This product is intended for research and analytical applications. Cyclobenzaprine hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
|
-
- HY-161836
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
α2AR agonist 1 (compound S6a), a new morpholine-containing pyrimidinone, acts as an agonist of α2-adrenoceptor. α2AR agonist 1 induces a concentration-dependent relaxation on aortic ring pre-contracted with Phenylephrine (HY-B0769; pEC50=6.81). α2AR agonist 1 increases NOx and NO levels in HUVECs .
|
-
- HY-15485
-
|
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
Cancer
|
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
|
-
- HY-101607A
-
|
Calcium Channel
|
Cardiovascular Disease
|
KT-362 free acid is an intracellular calcium antagonist with antiarrhythmic and vasodilatory effects. KT-362 free acid shows an antagonistic effect against norepinephrine (NE) induced vasoconstriction response, achieved by reducing inositol phospholipid hydrolysis, thereby reducing intracellular calcium mobilization. KT-362 free acid can be used to study the contraction and relaxation mechanisms of vascular smooth muscle, especially in exploring the role of intracellular calcium mobilization and inositol phospholipid hydrolysis in vascular contraction .
|
-
- HY-B0394R
-
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
|
-
- HY-126010
-
|
Piezo Channel
|
Others
|
Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca 2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .
|
-
- HY-B1205AR
-
|
mAChR
|
Cardiovascular Disease
Neurological Disease
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
- HY-B1640R
-
Etacrynic acid (Standard)
|
Glutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cancer
|
Ethacrynic acid (Standard) is the analytical standard of Ethacrynic acid. This product is intended for research and analytical applications. Ethacrynic acid (Etacrynic acid) is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice .
|
-
- HY-B0678
-
AHR438; NSC170959
|
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-123468
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-123468A
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-112348
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-B0678S
-
|
Isotope-Labeled Compounds
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
Metaxalone-d3 is the deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-W011269
-
EPA sodium; Timnodonic acid sodium
|
Endogenous Metabolite
Histone Demethylase
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation .
|
-
- HY-B0660
-
EPA; Timnodonic acid
|
Endogenous Metabolite
Histone Demethylase
|
Neurological Disease
Cancer
|
Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .
|
-
- HY-B0678S1
-
AHR438-d6; NSC170959-d6
|
Isotope-Labeled Compounds
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-B0740S3
-
MK130-d3-1 hydrochloride
|
Isotope-Labeled Compounds
5-HT Receptor
Parasite
|
Infection
Neurological Disease
|
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
|
-
- HY-B0660A
-
EPA (metformin); Timnodonic acid (metformin)
|
Endogenous Metabolite
Histone Demethylase
|
Neurological Disease
Cancer
|
Eicosapentaenoic Acid (EPA) metformin is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic acid metformin exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). EEicosapentaenoic acid metformin activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic acid metformin can promote relaxation of vascular smooth muscle cells and vasodilation .
|
-
- HY-B0678R
-
AHR438 (Standard); NSC170959 (Standard)
|
NF-κB
PGC-1α
|
Neurological Disease
Inflammation/Immunology
|
Metaxalone (Standard) is the analytical standard of Metaxalone. This product is intended for research and analytical applications. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
- HY-19927A
-
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .
|
-
- HY-N7690
-
|
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
- HY-B0660R
-
|
Endogenous Metabolite
Histone Demethylase
|
Neurological Disease
Cancer
|
Eicosapentaenoic Acid (Standard) is the analytical standard of Eicosapentaenoic Acid. This product is intended for research and analytical applications. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .
|
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-B0660S1
-
EPA 1,2,3,4,5-13C, FA 20:5-13C5
|
Isotope-Labeled Compounds
Endogenous Metabolite
Histone Demethylase
|
Neurological Disease
Cancer
|
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .
|
-
- HY-137325A
-
|
Calcium Channel
|
Metabolic Disease
|
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
|
-
- HY-125782
-
15(R)-15-Methyl PGD2
|
Prostaglandin Receptor
|
Metabolic Disease
|
15(R)-15-Methyl prostaglandin D2 (15(R)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1and CRTH2/DP2. 15(R)-15-Methyl prostaglandin D2 is a potent, selective agonist for the CRTH2/DP2 receptor. The EC50 values for eosinophil CD11b expression, actin polymerization, and chemotaxis are 1.4, 3.8, and 1.7 nM, respectively, each of which is approximately 3-5 fold lower than those for PGD2. In contrast the EC50 for the DP1-mediated increase in platelet cAMP by 15(R)-15-methyl PGD2 is >10 μM.
|
-
- HY-150979
-
|
Fluorescent Dye
|
Cancer
|
Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-150979
-
|
Fluorescent Dyes/Probes
|
Gd-NMC-3 is a near-infrared fluorescence/magnetic resonance (NIRF/MR) bimodal imaging probe. Gd-NMC-3 shows high resolution and sensitivity in tumor imaging with good biocompatibility, indicating huge application potential .
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Cat. No. |
Product Name |
Type |
-
- HY-W127670
-
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Cell Assay Reagents
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Decamethonium (iodide) is an organic compound containing ammonium and iodide ions. It is commonly used as a neuromuscular blocking agent in anesthesia to induce muscle relaxation during surgery. Decamethonium Iodide acts by binding to nicotinic acetylcholine receptors (nAChRs) in the neuromuscular junction, causing depolarization block and subsequent skeletal muscle paralysis. In addition, it can also serve as a reference standard for pharmacological studies of nAChRs.
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P0102
-
|
mAChR
|
Neurological Disease
|
Dipeptide diaminobutyroyl benzylamide diacetate, a Wagerlin-1-mimicking peptide, is a mAChR antagonist. Dipeptide diaminobutyroyl benzylamide diacetate can induce muscle relaxation .
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-
- HY-P1016B
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-3020 ammonium is a selective endothelin receptor (ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
|
-
- HY-P4766
-
|
CGRP Receptor
|
Cardiovascular Disease
|
Adrenomedullin (porcine) is a peptide that regulates vasodilation. Adrenomedullin (porcine) induces endothelium-dependent relaxation in rat aorta with IC50 value of 2.4 nM. Adrenomedullin (porcine) induces endothelium-independent relaxation of porcine coronary arteries with an IC50 of 27.6 nM .
|
-
- HY-P3562
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|
Peptides
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Others
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PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM .
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-
- HY-P10549
-
|
Endogenous Metabolite
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Neurological Disease
|
NGFFFamide is a muscle-active neuropeptide found in sea urchins. NGFFFamide regulates muscle activity by directly interacting with receptor proteins on muscle cells, or indirectly by stimulating nerves or other cell types to release muscle-active factors. NGFFFamide can be used to study muscle contraction and relaxation .
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-
- HY-P1016
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 1 2.
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-101952
-
-
-
- HY-N3488
-
-
-
- HY-N0484
-
-
-
- HY-W012980
-
-
-
- HY-N10495
-
-
-
- HY-N2646
-
-
-
- HY-N8444
-
-
-
- HY-169871
-
-
-
- HY-N10881
-
-
-
- HY-N1620
-
-
-
- HY-101952R
-
-
-
- HY-W012980R
-
-
-
- HY-N0485
-
-
-
- HY-N11538
-
-
-
- HY-B0394R
-
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
Atropine (sulfate monohydrate) (Standard) is the analytical standard of Atropine (sulfate monohydrate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate monohydrate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate monohydrate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate monohydrate can be used for research of anti-myopia and bradycardia .
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-
-
- HY-B1205AR
-
|
Alkaloids
Structural Classification
Other Alkaloids
Source classification
Atropa belladonna Linn.
Solanaceae
Plants
|
mAChR
|
Atropine (sulfate) (Standard) is the analytical standard of Atropine (sulfate). This product is intended for research and analytical applications. Atropine (Tropine tropate) sulfate is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with IC50 values of 0.39 and 0.71 nM for Human mAChR M4 and Chicken mAChR M4, respectively. Atropine sulfate inhibits ACh-induced relaxations in human pulmonary veins. Atropine sulfate can be used for research of anti-myopia and bradycardia .
|
-
-
- HY-W011269
-
-
-
- HY-B0660
-
-
-
- HY-N7690
-
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Metabolic Disease
Plants
Disease Research Fields
Zingiberaceae
|
Calcium Channel
|
3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
|
-
-
- HY-B0660R
-
-
-
- HY-N3945
-
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Infection
Alkaloids
Structural Classification
other families
Classification of Application Fields
Source classification
Plants
Isoquinoline Alkaloids
Glaucium flavum
Inflammation/Immunology
Disease Research Fields
Papaveraceae
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-101952S
-
|
Prostaglandin E2-d4 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
|
-
-
- HY-B0678S
-
|
Metaxalone-d3 is the deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
-
- HY-101952S1
-
|
Prostaglandin E2-d9 is the deuterium labeled Prostaglandin E2. Prostaglandin E2 (PGE2) is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation[1][2].
|
-
-
- HY-B1283S
-
|
Mephenesin-d3 is deuterium labeled Mephenesin. Mephenesin is an NMDA receptor antagonist. Mephenesin is also a central muscle relaxant with antianxiety, muscle-paralyzing and anticonvulsant effects. Mephenesin acts directly on the skeletal muscle fibres to produce skeletal muscle relaxation. Mephenesin is promising for research of spasticity or painful muscle spasm .
|
-
-
- HY-B0678S1
-
|
Metaxalone-d6 is deuterium labeled Metaxalone. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia .
|
-
-
- HY-B0740S3
-
|
Cyclobenzaprine-d3-1 hydrochloride (MK130-d3-1 hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride (HY-B0740). Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
|
-
-
- HY-B0660S1
-
|
Eicosapentaenoic acid 1,2,3,4,5- 13C5 (EPA 1,2,3,4,5- 13C, FA 20:5- 13C5) is 13C labeled Eicosapentaenoic Acid. Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation .
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